Results 121 to 130 of about 53,238 (282)

Epigenetic polypharmacology: from combination therapy to multitargeted drugs [PDF]

, 2016
The modern drug discovery process has largely focused its attention in the so-called magic bullets, single chemical entities that exhibit high selectivity and potency for a particular target.
A Anighoro, A Dey, A Ganesan, A Mai, A Nudelman, AF Fliri, B Al-Lazikani, B Knoechel, B Meunier, BC Smith, BC Smith, BC Smith, BE Gryder, C Choudhary, C Corminboeuf, C Liu, C Qian, C Tang, C Yu, C Zwergel, C-W Chen, CM Fillmore, CM Grozinger, CY Fong, D Bixby, D Gallenkamp, D Matei, D Passarella, D Rotili, D Sharma, DA Mele, E Bicaku, E Borretto, E Nicodeme, F Sun, F-W Peng, G Zhang, G-L Chen, GE Winter, GL Verdine, H Patel, HS Bandukwala, HS Takhar, J Fischer, J Lu, J Schneider, J Zhao, J Zuber, J-B Chen, J-F Couture, J-PJ Issa, JC Culhane, JL Avalos, JM Burg, JS Kirk, K Agger, K Chen, K K-p, K Pruitt, K Zhao, KB Daniel, KT Thurn, L Chen, L Chen, LK Gediya, M Buchwald, M De los Santos, M Yang, M Zuo, MA Dawson, MA Dawson, MA Park, MB Poulin, MC Chen, MJ Keiser, MM Singh, MS Finnin, N Geva-Zatorsky, OW Rokhlin, P Anand, P Bamborough, P Filippakopoulos, P Hu, P Hu, P Jones, P Rathert, PA Marks, PK Mazur, PN Munster, Q Wang, R Anand, R Morphy, R Morphy, R Nimmanapalli, R Pereira, R Pili, R Álvarez, RA Copeland, RA Juergens, RL Momparler, S Daujat, S Klimasauskas, S Mahboobi, S Mahboobi, S Zhao, SC Hodawadekar, SJ Atkinson, SS Ng, T Beckers, T Finkel, T Kokkola, T Qiu, T Vaissiere, T-G Lee, TH Luu, TJ Galloway, TM Pitts, W Guerrant, WF Hawse, X Cai, X Cheng, X Sun, X Zhang, Y Ling, Y Zhang, Z Chen   +125 more
core   +1 more source

OCTN2 Activates a Non‐Canonical Carnitine Metabolic Pathway to Promote MASH‐HCC Progression and Immunotherapy Resistance

Advanced Science, EarlyView.
In non‐MASH‐HCC, L‐carnitine promotes tumor progression primarily through its classical role in enhancing fatty acid oxidation (FAO). However, in MASH‐HCC, where FAO is markedly suppressed, L‐carnitine shifts from this canonical function to serve instead as an intracellular acetyl group buffer.
Chuqi Xia, Xiao Zhang, Jinze Li, Ning Xu, Sheng Hu, Qiyu Lu, Yuxuan Li, Taifu Xiao, Xu Li, Xue Wang, Kequan Xu, Daoming Liang   +11 more
wiley   +1 more source

Application of Small Epigenetic Modulators in Pediatric Medulloblastoma [PDF]

, 2018
Medulloblastoma is one of the most frequent among pediatric brain tumors, and it has been classified in various subgroups. Some of them already benefit from quite good therapeutic options, whereas others urgently need novel therapeutic approaches ...
Annalisa Romanelli, Antonello Mai, Antonello Mai, Clemens Zwergel, Giulia Stazi, Giuseppina Catanzaro, Marco Tafani, Sergio Valente, Zein Mersini Besharat   +8 more
core   +2 more sources

Histone deacetylase inhibitors as cancer therapeutics [PDF]

Annals of Translational Medicine, 2016
Cancer cells contain significant alterations in their epigenomic landscape, which several enzyme families reversibly contribute to. One class of epigenetic modifying enzymes is that of histone deacetylases (HDAC), which are receiving considerable scrutiny clinically as a therapeutic target in many cancers.
openaire   +2 more sources

Development of Dimethylsulfonium Probes for Broad Profiling of Methyllysine Reader Proteins

Advanced Science, EarlyView.
Development of oligoglycine‐based dimethylsulfonium probes for unbiased crosslinking to methyllysine readers. The general probe facilitates profiling of site‐specific methyllysine readers, evaluation of selectivity and activity of reader inhibitors, and global profiling of methyllysine readers.
Jinyu Yang, Yihang Xiao, Yingxiao Gao, Mingxuan Wu   +3 more
wiley   +1 more source

The human silent information regulator (Sir)2 homologue hSIRT3 is a mitochondrial nicotinamide adenine dinucleotide-dependent deacetylase. [PDF]

, 2002
The yeast silent information regulator (Sir)2 protein links cellular metabolism and transcriptional silencing through its nicotinamide adenine dinucleotide (NAD)-dependent histone deacetylase activity.
Frye, Roy A, North, Brian J, Ott, Melanie, Schwer, Bjorn, Verdin, Eric   +4 more
core  

Regulation of alphaherpesvirus infections by the ICP0 family of proteins [PDF]

, 2013
Immediate-early protein ICP0 of herpes simplex virus type 1 (HSV-1) is important for the regulation of lytic and latent viral infection. Like the related proteins expressed by other alphaherpesviruses, ICP0 has a zinc-stabilized RING finger domain that ...
Boutell, Chris, Everett, Roger
core   +1 more source

Macrophage TRIM21 Inhibition Ameliorates Murine Acute Pancreatitis via PHB2‐Mediated Mitochondrial Stabilization

Advanced Science, EarlyView.
Macrophage‐derived TRIM21 drives the progression of AP via ubiquitin‐proteasome‐mediated degradation of PHB2, leading to impaired PHB2‐mediated mitophagy. Therefore, accumulation of cytosolic mtDNA hyperactivates the cGAS‐STING signaling axis, thereby amplifying inflammatory cascades.
Yansong Xu, Yuansong Sun, Xin Zhou, Kai Song, Chunlin Yin, Zhaohua Wang, Fei Xie, He Li   +7 more
wiley   +1 more source

The Process and Strategy for Developing Selective Histone Deacetylase 3 Inhibitors

Molecules, 2018
Histone deacetylases (HDACs) are epigenetic drug targets that have gained major scientific attention. Inhibition of these important regulatory enzymes is used to treat cancer, and has the potential to treat a host of other diseases.
Fangyuan Cao, Martijn R. H. Zwinderman, Frank J. Dekker   +2 more
doaj   +1 more source

Chaperone‐Mediated Autophagic Degradation of USP9X in Macrophages Exacerbates Postmyocardial Infarction Inflammation and Cardiac Dysfunction

Advanced Science, EarlyView.
This study demonstrates that inflammatory stimuli induce the acetylation‐triggered, chaperone‐mediated autophagic degradation of ubiquitin‐specific peptidase 9 X‐linked (USP9X) in macrophages. USP9X acts as a macrophage “inflammation switch” after myocardial infarction (MI). USP9X loss destabilizes tumor necrosis factor receptor‐associated factor (TRAF)
Biqing Wang, Xiangheng Cai, Mengqi Li, Xue Liu, Junhui Xue, Ye Liu, Ding Ai, Xinyang Hu   +7 more
wiley   +1 more source